A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.

ABSTRACT:

Introduction

The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery. Traditional radioligand assays are labor-intensive, preventing their application at the early stages of drug discovery. Fluorescence-based assays offer several advantages, including a possibility to develop a homogeneous format, continuous data collection, and higher throughput. This study sought to develop a fluorescence-based binding assay to investigate ligand-binding kinetics at human cannabinoid type 1 and 2 receptors (CB1R and CB2R).

Methods

We synthesized D77, a novel tracer derived from the non-selective cannabinoid Δ⁸-THC. Using time-resolved Förster resonance energy transfer (TR-FRET), we developed an assay to study

SUBMITTER: Borrega-Roman L 

PROVIDER: S-EPMC12015242 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature